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Drug Discovery: Easing the Chemistry Bottleneck

contents >>>>>>>>>>>>>>>>>>>>> 3 Agenda

7 Speaker Biographies

13 Drug Discovery Sponsors

14 Notes

25 Evaluation

27 Save the Date: Drug Discovery Partnership

28 Registration Form

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KEY AREA FOR DISCUSSION The program is shaped to address key bottlenecks along the drug discovery process.This far-reaching discussion on some of the biggest challenges faced by the industry is designed to highlight technology trends as they emerge.

Conference Day One: Monday, 8th June 2009 7:30a CONTINENTAL BREAKFAST & REGISTRATION

8:15a CHAIRPERSON'S WELCOME & OPENING REMARKS Melvin Reichman, Ph.D., Director LIMR Chemical Genomics Center (LCGC), Lankenau Institute for Medical Research

8:30a COMPOUND MANAGEMENT'S ROLE IN ACCELERATING DRUG John J. Isbell, Ph.D., Director of Analytical Sciences and DMPK, Genomics DISCOVERY Institute of the Novartis Research Foundation ● Outline compound management's central role in drug discovery ● Discuss key responsibilities of compound management in supporting medicinal chemistry (i.e. accept and rearray compounds for all assays in assay-ready format; and perform LC/ MS analysis for all med chem.. solutions liquid handled) ● Understand ADME and liability assays, and their impacts on med chem., and ADME) ● Discuss the GNF solution and highlight critical part CM played in PK processing ● Use tracking and automation skills to make discovery processes more efficient

9:15a DEVELOPING A GLOBAL BIOLOGICS REGISTRATION SYSTEM Joseph M. Cesarone, Ph.D., Principal Research Computer Scientist, Scientific ● Defining biological entities and their rules for uniqueness; tracking the Informatics & Automation, Abbott Laboratories lineage of an entity and the relationships between entities ● Understanding and supporting diverse workflows across projects and sites ● Integrating with other Drug Discovery applications ● The Special Interest Group (SIG) model for collaborative development: Minimising project risks and costs

10:00a MORNING REFRESHMENT AND NETWORKING BREAK

10:15a PANEL DISCUSSION: COMPARE WORKFLOW FOR COMPOUND MODERATOR: MANAGEMENT Dr. Rodney A. Bednar, Senior Investigator and Chief Drug Discovery ● Identify the bottlenecks in compound processing/ workflow Engineer, Facility for Automation and Screening Technology (FAST), Merck (HTS compound support/ chemistry supply) Research Laboratories ● Understand your customers' needs and deliver compounds in a timely fashion PANELISTS: ● Discuss strategies to ensure turnaround time Janet Diratsaoglu, Head of Chemical Information and Compound Inventory ● Explore workflow options (workstation vs. integrated system; Lead ID Groups, Hoffman La Roche vs. Lead OP ) Scott D. Mosser, Senior Research Associate and Drug Discovery Manager, ● Review compound management and assay management Facility for Automation and Screening Technology (FAST), Merck Research ● Improve real time lead identification strategies Laboratories Dr. Sue Holland-Crimmin, Site Director, Sample Management Technologies, GlaxoSmithKline David Harding, Sales Director, RTS Life Science

11:15a CASE STUDY: ITERATIVE RANDOM AND FOCUSED SCREENING: A Suresh B. Poda, Ph.D., Senior Scientist, Lundbeck Research USA THOUGHTFUL APPROACH TO INCREASE HIT RATES ● Random screening using a small set of collection (20,000 compounds) that covers entire chemical space of the library ● 3-4 rounds of Iterative focused screening using computational modeling ● Improved hit rates with less resources

12:00p LUNCHEON

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1:15p CORNING EPIC® SYSTEM: A LABEL-FREE PLATFORM FOR HIGH Topics of the discussion include: THROUGHPUT DRUG DISCOVERY ● Principle of operation of the Epic System; The Epic System is a novel, label-free detection platform designed for both bio- ● Applications of the Epic System for cell-based GPCR screening; assay development and for high throughput drug discovery. Based on optical ● Applications in biochemical binding and functional assays for small biosensor technology, the system provides a high sensitivity label-free molecule and fragment based drug discovery; detection platform for measuring both molecular interactions in a biochemical ● Applications for biologic drug discovery; assay, as well as integrated cellular responses of endogeneous or over- expressed receptors in a cell-based assays. Detection of live cell and time Arron S. Xu, Ph.D., Manager, North America Epic® Applications Center, Corning dependent cellular response in a pathway unbiased manner with the Epic system may provide previously unattainable biological and pharmacological information for an integrated drug-stimulated cellular response. The SBS- standard 384 well Epic sensor plate enables the adaptation of the Epic system to HTS drug discovery.This presentation will introduce the principle of the Epic system and highlight its applications in drug discovery.

1:30p PRACTICAL APPLICATIONS OF LEAN THINKING PRINCIPLES IN Marybeth S. Burton, Associate Director, Chemical Technologies, Schering- COMPOUND MANAGEMENT Plough Research Institute ● Identify strategies to overcome the 'bottlenecks' ● Gain buy-in from clients for process change ● Implement workflow to minimize "non-value added" work

2:00p CASE STUDY ROUNDTABLE: STREAMLINING SAMPLE MANAGEMENT MODERATOR: PROCESS Edward W. Petrillo, Discovery Performance Strategies LLC Panelists will present case study describing how they utilize lean principal to deliver greater value in one or more of the areas listed below: Panelists: ● Safeguard integrity of compound collections John J. Isbell, Ph.D., Director of Analytical Sciences and DMPK, Genomics ● Deliver compounds to customers in timely fashion Institute of the Novartis Research Foundation ● Maintain capacity in response to rising demand Manori Turmel, Principal Scientist, AstraZeneca ● Operate at the highest possible efficiency in resource expenditure Marybeth S. Burton, Associate Director, Chemical Technologies, Schering- and capital investment Plough Research Institute

3:00p AFTERNOON REFRESHMENTS AND NETWORKING BREAK

3:30p PANEL DISCUSSION: STRATEGIES FOR OPTIMAL SCREENING LIBRARY MODERATOR: SIZE TO IMPROVE THE EFFICACY OF DRUG DISCOVERY Rick Hammar, Director, Compound Management, Chemistry and Screening ● Incorporates tractable chemistry to improve drug discovery process Services, ASDI Inc. ● Discuss selection on biologically annotated, IP-rich (novel), rationally designed, and privileged structure molecules PANELISTS: ● Explore whether screening library as small as 10,000 compounds is Ricardo Macarrón, EMTM, Ph.D.,VP of Sample Management Technologies, capable of producing better results GlaxoSmithKline Dave Schultz, Ph.D., Director, Protein Production, Libraries & Molecular Screening Facility,Wistar Scientist, Wistar Institute

4:30p AUTOMATION FROM COMPOUND STORAGE TO ASSAY DEVELOPMENT Dalin Nie, Head of Compound Management, AstraZeneca ● Sample storage and retrieval with the ability to randomly access up to 30,000 samples daily ● Produce assay plates in nanoliter volumes on demand for HTS ● Minimize delivery time to less than 48 hours ● Integrate compound management into drug discovery process with full support to lead identification and lead optimization

5:15p COCKTAIL RECEPTION

Conference Day Two: Tuesday, 9th June 2009 7:30a CONTINENTAL BREAKFAST & REGISTRATION

8:15a CHAIRPERSON'S WELCOME & OPENING REMARKS Melvin Reichman, Ph.D., Director LIMR Chemical Genomics Center (LCGC), Lankenau Institute for Medical Research

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8:30a NARROWING INTERFACE BETWEEN LEAD DISCOVERY & OPTIMIZATION MODERATOR: ● Thinking backwards: Drug-like to lead-like and back Melvin Reichman, Ph.D., Director LIMR Chemical Genomics Center (LCGC), ● On-target structure activity relationships (SAR): It's a wide world of Lankenau Institute for Medical Research catalog diversity ● Off-target structure liability relationships (SLR): A side effect around PANELISTS: every coronary Li Tao Zhang, Executive Director, Lead Evaluation and Mechanistic ● Lead exploration to lead development: How many roads to CROss Biochemistry, Bristol-Myers Squibb ● Project Management:When to hold and when to fold; who makes the call? Jonathan Usuka, Senior Director of Industry Marketing, Accelrys

9:30a QUANTIGENE: SINGLE AND MULTIPLEX GENE EXPRESSION SOLUTIONS Dr. Gary McMaster, Chief Scientific Officer, Affymetrix FOR DRUG DISCOVERY AND DEVELOPMENT ● QuantiGene multi-format gene expression technology platform can be used throughout the drug discovery pipeline from primary- and secondary screening, through toxicology, biomarker discovery and companion diagnostics. ● QuantiGene bead-based multiplex assay enables a novel approach to compound screening by plexing both genes and samples directly from cell lysates thereby substantially increasing throughput to a level that gene signatures can be made from primary screens.This assay is rapid, sensitive, and allows high throughput gene expression analysis without extensive optimization. ● QuantiGene ViewRNA in situ gene expression technology is capable of measuring single RNA molecules in individual cells.The automation-friendly 384 well format has a simple assay workflow that is suitable for high- throughput applications such as phenotypic- or reporter gene screening. ● QuantiGene precisely measures RNA expression directly from cell lysates and tissue homogenates utilizing a unique reporter signal amplification system, eliminating variations or errors inherent to extraction, reverse transcription and amplification of target molecules. ● QuantiGene singleplex - and multiplex assay applications include microarray validation, compound- and RNAi screening and biomarker analysis from multiple matrices including tissue, blood, and Formalin Fixed Paraffin Embedded (FFPE) archived samples.

10:15a MORNING REFRESHMENTS AND NETWORKING BREAK

10:30a ADME AND THE CHEMISTRY BOTTLENECK - FROM HTS TO Norman Huebert,Team Leader Discovery ADME, Johnson & Johnson PHARMACOKINETICS ● HTS in vitro assays can be important steps in designing out unwanted pharmaceutical properties ● The HTS in vitro models should be linked to more complex in vitro and in vivo models so as to facilitate simulation and 'prediction' ● Higher throughput approaches to target engagement and in vivo PK properties can speed up candidate selection in later LO phases ● The choice of appropriate in vitro or in vivo models should be based on chemotype and not on one-size-fits-all.

11:15a COMPUTATIONAL DRUG DISCOVERY: INTEGRATING A COLLABORATIVE Sean Ekins, Ph.D., D.Sc., Collaborations Director, Collaborative Drug DATABASE Discovery Inc. ● Learn about the use of computational models for PXR and other ADME/ Tox properties ● Learn how a web-based database can foster collaborations in drug discovery

12:00p LUNCHEON

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1:15p PROVIDING HIGH QUALITY AND EFFICIENT SUPPORT FOR THE DIVERSE Robert Cain, Manager R&D IS, Allergan ANALYTICAL WORK-FLOWS IN PHARMACEUTICAL DISCOVERY In a pharmaceutical discovery organization, scientists carry out diverse sets of complex assays many of which require their own highly sophisticated visual and statistical analyses. Allergan recently instituted a research analytics program that has developed certain principles to efficiently support these analyses. ● There is no substitute for a well-structured data warehouse and data mart ● Identify common requirements and automate them in intuitive ways ● Let scientists focus on science not data handling ● Train scientists with their data

2:00p TECHNOLOGY ROUNDTABLE Case studies presented by table facilitators and attendees will serve as the basis for discussion at each table. Attendees will be allowed to attend (2) table discussions within this hour to allow for greater information sharing. TABLE 3: THE USE OF ECHO® ADE TECHNOLOGY FOR IMPROVING TABLE 1: CORNING EPIC® SYSTEM: A LABEL-FREE PLATFORM FOR HIGH COMPOUND MANAGEMENT THROUGHPUT DRUG DISCOVERY Mark Lasinski, Senior Director, Global Sales, Labcyte Arron S. Xu, Ph.D., Manager, North America Epic® Applications Center, Corning Table 4: CyBio innovations in liquid handling help drive low volume and high density screening efforts. A sneak peek into CyBio's future TABLE 2: TODAY'S CHALLENGES AND RESPECTIVE SOLUTIONS IN developments COMPOUND MANAGEMENT SOFTWARE Ian Hanegraaf, General Manager, CyBio Michael Girardi, President, Titian Software

3:00p AFTERNOON REFRESHMENTS AND NETWORKING BREAK

3:30p EXPLORE THE UNIQUE CHALLENGE FACED BY ACADEMIA Melvin Reichman, Ph.D., Director LIMR Chemical Genomics Center (LCGC), ● Target novelty: Publish or patent Lankenau Institute for Medical Research ● The NIH Roadmap: Biomedical highway to the future--or bridge to nowhere? ● 'Probing' the boundaries between basic and applied research ● 'Re-Purposing:Truly a panacea? ● 'Better drugs through better chemistry: Huh?

4:15p PANEL DISCUSSION: TEAMING UP TO TAME THE BOTTLENECK: MODERATOR: INDUSTRIAL-ACADEMIC INTERACTIONS Dr. Rathnam Chaguturu, Director, High Throughput Screening ● 'Pharma-Academic partnerships: Devil (God) is in the details Laboratories, University of Kansas ● 'Changing Pharma-Academia landscape: Grants, contracts and collaboration PANELISTS: ● 'Role of Academia in translational research: Conquering the valley Krishna Kodukula, Ph.D., Executive Director, Center for Advanced Drug of death Research, SRI International ● 'Role of academic technology transfer offices: Bridging the great divide Jim Baxendale, Executive Director-KU Center for Technology ● 'Explore opportunities for collaboration between Pharma, academia Commercialization, University of Kansas and the Government:The time is now Wei Zheng, Ph.D., Group Leader, Cellular Signaling Assays, NIH Chemical Genomics Center Jeff Dodge, Ph.D., Research Fellow, Academic Research Liaison, Eli Lilly Katya Tsaioun, Ph.D., President, Scientific Director, Apredica Jia Xu, Ph.D., Director of Operations, Johns Hopkins University School of Medicine

5:15p CLOSING REMARKS AND END OF CONFERENCE

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James G. Baxendale MS, MBA, Executive Director, UNIVERSITY OF KANSAS Jim has worked for over thirty-five years in the Kansas City biomedical community. Currently, he serves as the Executive Director of the KU Center for Technology Commercialization with responsibility for the intellectual property of all the University of Kansas campuses. Jim's responsibilities include the commercialization of faculty research by securing patents, trademarks and copyrights, negotiating licenses, research agreements, confidentiality agreements and material transfer agreements. He also assists the management staff of spin-off companies created from the University of Kansas technologies. Prior to joining the University of Kansas, Jim was Vice-President of Operations for Regional Media Laboratories. Earlier, he served as their Director of Research & Development and Supervisor of Quality Control. In addition, Jim has held management positions in hospitals and private clinical laboratories throughout the Greater Kansas City Area. Jim holds a Bachelor of Science Degree in Medical Technology, a Master of Science in Microbiology from the University of Missouri-Kansas City, and an MBA from the Rockhurst University Executive Fellows MBA Program. For the Association of Medical Device Manufacturers, in Washington, D.C., Jim served as a member of the Board of Directors, Secretary and President. He was appointed by the Commissioner of the Food and Drug Administration to the Medical Device Good Manufacturing Practices Advisory Committee for a 4-year term. Jim served as Chairman of the Silicon Prairie Technology Association BioScience Network Steering Committee for four years, and functioned as a Business Counselor, Instructor and Consultant for the Kauffman Foundation Fast Trac program for a period of 7 years.

Dr. Rodney A. Bednar, Senior Investigator, Group Leader, Chief Drug Discovery Engineer, FACILITY FOR AUTOMATION AND SCREENING TECHNOLOGY (FAST) MERCK RESEARCH LABORATORIES Dr. Rodney A. Bednar, has worked for Merck & Co., Inc. in their West Point Pennsylvania Research Laboratories for the last 18 years. He is a Senior Investigator and the Chief Drug Discovery Engineer and founder of FAST. FAST, an acronym that stands for Facility for Automation and Screening Technology. His group has served to transform the Drug Discovery Process at Merck. Prior to joining Merck, Rodney enjoyed a successful academic career at the SUNY Stony Brook, where he maintains an adjunct appointment. While a Professor in the Department of Pharmacological Sciences and in the Department of Chemistry his laboratory contributed to our understanding of Perfection in Enzyme Catalysis. Rodney was highly regarded for his training of undergraduate, graduate and postdoctoral students in art of scientific research and he supported the Stony Brook Medical Schools as the Pharmacology Course Director for 8 years.

Marybeth Burton, Associate Director, Chemical Technologies, SCHERING-PLOUGH RESEARCH INSTITUTE Marybeth Burton is responsible for management of the collection of proprietary research samples at Schering-Plough Research Institute (SPRI). Ms. Burton's responsibilities include oversight of compound acquisition, compound inventory and request fulfillment, compound collection integrity and enhancement, and chemical reagent tracking. In addition, Ms. Burton manages the selection and implementation of new technologies and data management systems in the compound management area. Ms. Burton holds a B.A. in Biology and an M.S. in Information Science.

Contact information: 2015 Galloping Hill Rd K-15-4, 4920 Kenilworth, NJ 07033 [email protected] Tel: 908 740 7359 Fax: 908 740 7115

Robert Cain, Manager, ALLERGAN Robert Cain is a manager at Allergan where he supports drug discovery teams by managing the research analytics program which provides a research data warehouse, various customized applications and user support. He received his Ph.D. at the University of Michigan in 1997 where he studied NMR of macromolecules. After a two year post-doc and NCSU, he became manager of the Allergan chemistry spectroscopy group in 1999. Over the next few years his group took over responsibility for the Allergan chemical registration systems and began support discovery by federating various assay data sources using ISIS technology and Spotfire. The experience gained from these attempts led to the Research Data Warehouse project, which integrates all the major lead discovery databases at Allergan into 3rd Normal form data warehouse and a dimensional data mart. His team designed a custom web reporting tool that feature a novel search tools that allows scientists to intuitively create sophisticated queries and design custom reports. He will be talking about his team's current emphasis, which is to allow Allergan scientists to use the latest statistical & visual analytics tools to make the best decisions from their data.

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Joe Cesarone, Principal Research Computer Scientist, ABBOTT LABORATORIES Joe Cesarone is currently a Principal Research Computer Scientist at Abbott Laboratories, which he joined in 1991. He has 18 years experience in the design and development of enterprise applications for drug discovery. Areas of focus have included small molecule registration and inventory systems, gene and target knowledge databases, data mining of sequence databases and text mining of the biomedical literature, as well as the integration of systems across R&D. Most recently Joe has been the project manager for Abbott's global biologics registration system. He holds a B.S. in Chemistry from the University of Illinois at Urbana-Champaign and a Ph.D. in Organic Chemistry from Northwestern University, where he worked in the laboratory of Richard Silverman.

Dr. Rathnam Chaguturu, Executive Director, UNIVERSITY OF KANSAS Dr. Rathnam Chaguturu is the Executive Director of the High Throughput Screening laboratory at the University of Kansas (Lawrence, Kansas), and co-ordinates drug discovery activities across all academic campuses within the state of Kansas. He has more than 30 years of experience in new lead discovery and development, executing high throughput screens, and managing hit to lead projects. He joined Rutgers University in 1976 as an Assistant Professor of Biochemistry, and later moved to Dow Chemical Company-Central Research Laboratories as a Project Leader. At Dow, Rathnam instituted the first principles of chemical library screening for new lead discovery, and developed tools for mining in-house chemical archives. Rathnam joined Sierra Sciences as Director of Drug Discovery in 2006 after a 22-year outstanding career at FMC Corporation where he led discovery research efforts focused on ion channel, receptor, enzyme and cell-based targets, and instrumental in designing the industry-first Zymark robotic screening platform for new lead discovery. He recently organized a well-received workshop on high throughput screening (HTS) strategies in drug discovery, the first of its kind, in Panama City (Panama) aimed at Latin American scientists interested in drug discovery from natural sources. As a representative of FMC, he was one of the founding members of the Society for Biomolecular Sciences. He is currently on the executive board of the Midwest chapter of the Laboratory Robotics Interest Group as Academic Screening Chair. Dr. Chaguturu has authored over 45 research publications including reviews and book chapters, and holds 11 US patents.

Janet Diratsaoglu, Head of Chemical Information and Compound Inventory Groups, HOFFMAN LA ROCHE Janet Diratsaoglu completed her B.S. degree and M.S. degree in chemistry at the University of Karlsruhe in Germany. She joined Roche Nutley in 1989 as an assistant information scientist and became the head of chemical information services in 1994. In 1997, she was appointed to head the chemical information and the compound inventory management groups in Nutley in support of chemistry, oncology, metabolic diseases and HTS groups in research.

Jeffrey A. Dodge, Research Fellow, LILLY RESEARCH LABORATORIES Jeffrey A. Dodge received a BS in Chemistry in 1984 at Eckerd College in St. Petersburg, Florida. In 1989, he completed his PhD at University of California, Irvine in the field of molecular recognition. He joined Eli Lilly and Company in 1991 after postdoctoral studies at the University of Texas, Austin. Dr Dodge has extensive expertise in nuclear receptors, particularly in the area of selective estrogen receptor modulators and their application to women's health where he has published broadly. He is currently a Research Fellow at Lilly Research Laboratories.

Sean Ekins, Collaborations Director, COLLABORATIVE DRUG DISCOVERY INC. Sean Ekins graduated from the University of Aberdeen; receiving his M.Sc., Ph.D. and D.Sc. He was a postdoctoral fellow at Lilly Research Laboratories. He has worked as a senior scientist at Pfizer, Senior Computational Chemist at Lilly Research Laboratories, Associate Director of Computational Drug Discovery at Concurrent Pharmaceuticals, Inc. and Vice President of Computational Biology at GeneGo. Sean is currently working with several early stage companies including Collaborations in Chemistry Inc, Collaborative Drug Discovery Inc. and Arnold Consultancy and Technology LLC. He is also Adjunct Associate Professor, School of Pharmacy Department of Pharmaceutical Sciences, University of Maryland and Adjunct Professor in the Department of Pharmacology at University of Medicine and Dentistry of New Jersey - Robert Wood Johnson Medical School, Piscataway, NJ. He is on the scientific advisory board for Emiliem Inc., ChemSpider, Assay Depot and the advisory board for Chemical Informatics at Indiana University and editorial boards of the Journal of Pharmacological and Toxicological Methods, Drug Metabolism and Disposition, Drug Discovery Today, Pharmaceutical Research, Mutation Research Reviews and the ChemSpider Journal of Chemistry. He has authored or co-authored >130 peer reviewed papers and book chapters as well as edited three books on computational applications in pharmaceutical R&D and computational toxicology. His areas of interest are in vitro and computational ADME/Tox, systems biology, cheminformatics and computer-aided drug discovery.

Rick Hammar, National Sales Manager, Director, Compound Management, Chemistry and Screening Services, ASDI INC. Mr. Hammar joined ASDI Inc. in January 2003 and is responsible for developing ASDI's market depth and breadth in outsourced sample preparation service contracts. He is considered an expert in outsourcing compound management services. He played a key role in the launch of ASDI's reactive intermediate provision service business model, signing on 24 major pharmaceutical and biotechnology clients within the first 12 months. His 19 years of drug discovery sample preparation experience are essential to identifying viable outsourcing opportunities for potential clients, defining appropriate functional specifications, and liaising between client and ASDI project leaders to continually support the changing needs of research. Prior to joining ASDI, Mr. Hammar was employed for four years at Tomtec, Inc., a global research instrumentation provider, as the Director of Business Development and New Applications. Prior to that, Mr. Hammar worked for 10 years as Manager of the Compound Management and Distribution

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(Rick Hammar continued...) Department for Bristol Myers Squibb. He was instrumental in reformatting the existing compound collections to support the advent of High Throughput Screening at BMS, and later oversaw the centralization of storage and distribution at the Wallingford site, supporting seven domestic and international research facilities and multiple collaborations. He was the project manager for the BMS "Haystack" project, the installation and implementation of the world's largest Automated Storage and Retrieval System for research samples, and a central piece of a $43 M capital project. Mr. Hammar has attended the University of Connecticut MBA program and has earned his undergraduate B.S. in American Studies with a minor in business management from Central Connecticut State University. Contact information: [email protected] 601 Interchange Boulevard (T) 302.293.5766 Newark, DE 19711 (F) 302.266.8296

David Harding, Sales and Marketing Director, RTS LIFE SCIENCE He is a chartered engineer with a degree in Electronic and Control Engineering from the University of Hull, UK. David has worked on a range of automation applications, starting at Thorn EMI's Central Research Laboratories, Hayes, UK, where he worked on the automated assembly of consumer goods. At RTS he has worked on applications ranging from autonomous nuclear power reactor inspection to automated soup production. For the last 14 years David has focused on automation for life science research applications and, in particular, Sample Management.

Dr. Sue Holland-Crimmin, Site Head and Director of Sample Management Technologies, GSK PHILADELPHIA Dr Sue Holland-Crimmin is Site Head and Director of Sample Management Technologies at GSK Philadelphia. She is WW leader for Quality Initiatives and coleader of Automation & Technology within GSK SMTech. She has worked in areas of Sample Management, HT Screening and IT during here career which has spanned 3 countries and major sites within the GSK operation. She holds a PhD in Biochemistry & Genetics and a BSc in Microbiology and is a trained Lean Sigma facilitator.

Norman D. Huebert, Ph.D., Team Leader ADME, JOHNSON & JOHNSON PRD Dr. Huebert received a B.Sc. (Honours) degree in Biochemistry from the University of Saskatchewan in Saskatoon in 1974. He went on to complete his Doctor of Philosophy in Biological Psychiatry in the Neuropsychiatric Research Unit of the Department of Psychiatry at the same University in 1980. Following his formal training, he joined the Richardson Merrell Research Centre in Strasbourg, France in 1980 in the Pharmacokinetics Group of the Clinical Pharmacology Department. In 1996, Dr. Huebert transferred to the Aventis Research Centre in Bridgewater, NJ where he remained until joining 3-Dimensional Pharmaceuticals in 2001 as Director of the Analytical Chemistry and Pharmacokinetics Department. Dr. Huebert's efforts during his time with Aventis Pharmaceuticals were deployed in the support of Discovery and Development research programs through the application of in vitro and in vivo experimentation and the Development of Clinical Candidates through Pharmacokinetic support of clinical development programs. His initial interests in bioanalytical methodology and techniques and in vivo pharmacokinetics gradually developed in parallel with that of the industry to the investigation of in vitro techniques for the rapid prediction of pharmacokinetic parameters and the screening of large numbers of NCE's as a substitute for in vivo experimentation. He is currently Team Leader for ADME for the US RED site of Johnson and Johnson PRD and continues his interests in the use of in vitro and in vivo techniques to accelerate the advancement of discovery research programs and their successful progression into the formal development process. Contact information: 665 Stockton Drive Suite 104 Exton, PA 19341 [email protected]

Ricardo Macarron, Ph.D., VP of Sample Management Technologies, GLAXOSMITHKLINE Dr. Macarron is Vice-President of WW Sample Management Technologies in GlaxoSmithKline R&D. He recently served as President of the Society for Biomolecular Sciences (SBS) (2007-2008) and is Associate Editor of the Journal of Biomolecular Screening. He is the author of more than 50 publications on the field of biochemistry, lab automation and biomedical research. He joined GSK in 1992, and has been working since in positions of growing responsibility within the area of drug discovery (high throughput screening -HTS-, biological assay development and compound management). In his current position Dr. Macarron leads a group responsible for the storage and distribution of all chemical compounds tested in GSK drug discovery efforts. This global department employs 100 scientists located in 4 sites in 3 countries (USA, UK, Spain). Macarron received both his doctorate in Biochemistry and bachelor's degrees in Biology from the University Complutense of Madrid (Spain). Dr. Macarron also holds a master's degree in Technology Management from University of Pennsylvania.

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Gary McMaster, Ph.D., Chief Scientific Officer, AFFYMETRIX Gary brings more than 25 years of experience in drug discovery research and life science technologies to Affymetrix, holding senior management positions at Panomics and a number of leading pharmaceutical companies. Prior to being Chief Scientific Officer at Panomics, Gary was Director of Target Discovery at Eli Lilly; responsible for defining and implementing the company's research technologies and systems biology programs, including the integration of novel life science technologies for the company's target discovery research. Previously, he was Senior Director of Molecular Biology for Parke-Davis and Pfizer, where he oversaw the application of technologies and genomics research for drug discovery. Gary also spent 10 years at Ciba-Geigy and Novartis. During his tenure there, he held positions of increasing responsibility including Head of CNS Molecular and Cell Biology and Head of Neurodegenerative Diseases. His leadership experience also includes research management positions at the Max-Planck Institute for Immunology and Hoffman-La Roche Pharmaceuticals. Gary received his doctorate in developmental biology from the Swiss Institute for Experimental Cancer Research and is an author of more than 50 peer-reviewed scientific publications and numerous world and United States patents.

Scott Mosser, Senior Research Associate and Drug Discovery Manager, MERCK RESEARCH LABS My career has been dedicated to identifying novel, efficacious medicines so people can live long and prosperous lives. My earlier years were spent at the bench manually suspending compounds and producing dose inhibition profiles for tens of thousands of compounds. As technologies became available, I wanted to create a workflow that would incorporate the new emerging technologies and help the bench scientist do their job more efficiently and accurately. Over the last 10 years I have been involved in building a facility for automation and screening technologies with a goal to transform drug discovery at Merck Research Labs. The key to this transformation has been the development of lean workflows which enable us to support a steady state pipeline flow of high value small molecules through Lead ID and Lead OP phases of drug discovery. In order to accomplish this fete, we had to assemble a group of top notch, flexible and innovative experts in three core areas: robotic automation, assay informatics and biological screening. It has been my privilege to help build and manage this team to realize the benefits of using integrated robotic systems, work stations and our laboratory information management system.

Dr. Dalin Nie, Head of Compound Management & Automation, Associate Director of HTS & Global Support, ASTRAZENECA R&D Since joined AstraZeneca in the year 2000, Dalin has successfully defined & implemented the compound management and automation processes and established the compound management and automation capability at Wilmington. He designed, managed, established, and enabled the Wilmington Automated Compound Management Facility (ACMF), which is serving multiple research sites in several countries Dalin has been working in the Drug discovery Automation for over 13 years. He is currently the Chair of the Philadelphia Chapter of the Laboratory Robotic Interest Group (LRIG).

Edward W. Petrillo, Founder, DISCOVERY PERFORMANCE STRATEGIES, LLC Ed Petrillo began his career at BMS working on captopril, the first orally active ACE inhibitor. He advanced seven candidates toward the clinic, and invented Monopril , which reached $400 million in annual sales. In 1995 he began a career focus on novel technologies for drug discovery. The BMS team developed a commercially-successful array synthesis reactor and a comprehensive PreClinical Research Information System (PCRIS). As Vice President of New Leads, he oversaw the integration of HTS, compound distribution, combinatorial chemistry, and compound liability profiling. In 2004, Ed was appointed Distinguished Research Fellow, Discovery Technology. He pioneered the application of "Lean Thinking" to improve drug discovery productivity. Ed was awarded the Bristol-Myers Squibb Pharmaceutical Research Institute's Ondetti & Cushman Career Achievement Award in 2005. He retired in 2006 to found Discovery Performance Strategies, LLC, delivering consulting services to pharma and technology clients. Ed and his wife Joan reside in Pennington, New Jersey and enjoy summers at the nearby Jersey shore. Their children have all pursued careers in science and engineering- Daniel, chemistry; Laura, medicine, and David, mechanical engineering. For the past 10 years Ed's main pastime has been mentoring high school students in the FIRST (For Inspiration and Recognition in Science and Technology) Robotics program, a nationwide competition that encourages interest in technical careers.

Suresh Poda, Senior Scientist, LUNDBECK RESEARCH Suresh Poda (PhD, biochemistry), is a senior scientist at the HTS Center for Lundbeck Research in Paramus, NJ. After completion of his PhD in 1996, he did his postdoctoral research at University of Michigan, Ann Arbor, MI. In 2000, he started his pharmaceutical career at Astra Zeneca R&D, Montreal as a Scientist. His Joined Lundbeck in 2004, where he started working in the area of compound management and HTS. Lundbeck focuses on CNS disorders. While the primary targets are GPCRs, the company also focuses on other targets that are involved in neurotransmitter and neuro-inflammatory pathways.

Dr. Mel Reichman, Director, LANKENAU INSTITUTE FOR MEDICAL RESEARCH (LIMR) - CHEMICAL GENOMICS CENTER (LCGC) Dr. Mel Reichman received his Ph.D. in Neuroscience from the University of Rochester under a NRSA Fellowship, and did his postdoctoral studies as NRSA-NIDA Fellow at the Department of Pharmacology, University of Wisconsin Medical School at Madison. Dr. Reichman has held several leadership positions directing new leads discovery at leading pharma, including: G.D. Searle/Monsanto, Berlex Biosciences/Schering AG, Ligand

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Drug Discovery: Easing the Chemistry Bottleneck June 8-9, 2009

(Dr. Mel Reichman continued...) Pharmaceuticals, OSI Pharmaceuticals and DuPont Pharma. Dr. Reichman is presently Senior Investigator and Director of the Lankenau Institute for Medical Research-Chemical Genomics Center (LCGC), in Wynnewood, PA (www.LIMR.org). He serves as a reviewer on several NIH 'Roadmap' study sections and is an ad hoc consultant for regional biotech and technology companies. He is presently Director of the Lankenau Institute for Medical Research (LIMR)-Chemical Genomics Center (LCGC).

David C. Schultz, Ph.D., Wistar Scientist, THE WISTAR INSTITUTE Dr. Schultz received his Bacheor's of Science in Biochemistry from Albright College and a Master's of Science and Ph. D. in Chemistry from Lehigh University. His thesis research identified OVCA1/DPH2L1 a candidate tumor suppressor gene within a critical region of the genome that is frequently deleted in many carcinomas, including breast and ovarian cancers. During a post-doctoral fellowship at the Wistar Institute, he pioneered studies that defined basic mechanisms of transcriptional repression by the vertebrate specific KRAB-zinc finger protein family of trascription factors and the role they have in regulation of chromatin structure and epigenetic control of gene expression. He extended this work as an Assistant Professor in the Department of Pharmacology at Case Western Reserve University, where he focused on the role KRAB-zfp regulation of transcription in muscle satellite cell differention, mammary gland development and Hematopoietic stem cell biology. He returned to the Wistar Institute as a Senior Staff Scientist and Director for the Protein Expression, Libraries, & Molecular Screening Facility, where he has been vital to the development of Wistar's strategic effort to develop high-throughput screening and a research program in Chemical Biology and Translational Medicine. He is also a very active participant in a multi-institutional program project focused on Epigenetics in Ageing and age related pathologies. He is a broadly trained scientist in the areas of molecular biology, protein biochemistry, pharmacology, and genetic & epigenetic mechanisms of gene expression. His work in these areas has been published as original articles in Genes & Development, Embo Journal, Cancer Research, and Molecular and Cellular Biology.

Katya Tsaioun, Ph.D., Founder and President, APREDICA Dr. Tsaioun is founder and President of Apredica. Apredica specializes in rapid preclinical in vitro assessment of the ADME Tox (Absorption, Distribution, Metabolism, Elimination and Toxicity) properties of small-molecule and peptide therapeutics. Under Dr.Tsaioun's leadership Apredica has grown from 1.5 to 9 FTEs in less than 3 years and now is working with over 60 customer companies world-wide, ranging from academic institutions and virtual companies to large multinational pharmaceutical organizations. Apredica has established its reputation as a premiere innovation-driven drug-discovery contract research organization. 80% of Apredica's staff have Ph.D., and each has over 10 years of discovery experience. Apredica provides this expertise as an extension of client companies' R&D. Prior to founding Apredica, Dr. Tsaioun worked as a Group Leader at Surface Logix, where she built a team and developed a complete in vitro ADME and in vivo DMPK (drug metabolism and pharmacokinetics) program, which were a central part of the company's technology platform for optimizing and advancing drug leads in CNS and oncology therapeutic areas. Her group developed and validated a number of in vitro assays that became secondary screens in lead optimization such as BBB screen. This ADME program was instrumental to the 3 IND submissions which occurred within 9 months of establishing the in vitro ADME program. Prior to Surface Logix, Dr. Tsaioun worked at Mitotix (subsequently merged into GPC Biotech), where she pioneered cell-based assay development in the area of angiogenesis (oncology) and infectious disease. She gained expertise in assay validation, transfer to automation, running compound- library screens, and managing hit-to-lead and lead-optimization programs. While at GPC Biotech, Dr. Tsaioun managed the outsourcing of a battery of in vitro ADME assays and introduced and pioneered the establishment of in-house in vitro ADME capabilities, developing and validating a high-to- medium-throughput ADME assay panel and bringing in house in silico ADME prediction models. Dr. Tsaioun earned her M.S. degree in solid-state chemistry from the Leningrad Institute of Technology, and her Ph.D. from Tufts University. Her Ph.D. thesis on effects of signal transduction and apoptosis factors in the rat brain was done under direction of Drs. James Sadowski and James Joseph in the Neuroscience Laboratory. She completed her academic training in the Neurochemistry Department at the Harvard University Primate Center, working on in vivo and in vitro drug-dependence models with cannabinoid receptor and dopamine transporter systems. Dr. Tsaioun is active in many local and international professional and business societies such as AAPS, ACS, WEST, HBA, and the MIT Enterprise forum. She was invited to serve as a judge in the Yale Entrepreneurship Society's 2007 and 2008 business plan competitions. Dr. Tsaioun serves on the Scientific Review Boards of Alzheimer's Drug Discovery Foundation and International Rett Syndrome Foundation. Dr. Tsaioun is regularly interviewed by trade publications such as Genetic Engineering News, Drug Discovery Technology, and invited to speak at conferences on the topics of early toxicity assessment, building productive R&D teams, and entrepreneurship.

Manori Turmel, Principal Scientist, ASTRAZENECA Manori Turmel graduated with a BEng in Electrical and Electronic Engineering from the City University in London, UK. She received her PhD in Process Control Engineering from the Liverpool John Moors University in UK and completed her Post Doctorate Fellowship at the University of Strathclyde in Glasgow, UK. She joined AstraZeneca Pharmaceuticals in 2001, and is currently a Principal Scientist with the Compound Management and Automation group in AstraZeneca Discovery in Wilmington. She has played a key role in setting up the AstraZeneca Automated Compound Management Facility, and has recently been involved in a number of process improvement activities within the Drug Discovery phase. Her interests are Compound Management, Lab Automation, System Integration, Project Management and Business Process Analysis, Design & Improvements. She currently holds a Green Belt certification in Lean Six Sigma.

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Drug Discovery: Easing the Chemistry Bottleneck speaker biographies >>>>>>>>>>>>>>>>>>>>> >

Arron S. Xu, Ph.D., Manager, North America Epic® Applications Center, CORNING Arron received his Ph.D. in physical biochemistry from the Department of Biochemistry, University of Sydney, Australia with Prof. Philip W. Kuchel, in 1993. Following his Ph.D., he undertook a postdoctoral fellowship at the Australian Cooperative Research Centre for Molecular Technology from 1993 to 1995, and a NIH Fogarty International Visiting Fellowship at the Laboratory of Structural Biology, National Institute of Environmental Health Sciences from 1995 to 1998. This was followed by a research faculty post at the University of North Carolina-Chapel Hill before joining Ciphergen Biosystem Inc as a scientist and later as scientific program manager. He is currently the manager of the North America Epic®Applications group, Corning Life Sciences. Arron has worked on several areas of research with focuses on cellular membrane transport by NMR, membrane/ion channel biosensor by impedance spectroscopy, protein engineering, biodegradable scaffold for liver tissue engineer, clinical biomarker proteomics by mass spectrometry, and most recently in assay and applications of Epic®technology. He currently manages a team of application scientists for application development and supports centered around the Corning Epic®technology.

Jia Xu, Ph.D., Operation Director, JOHNS HOPKINS ION CHANNEL CENTER (JHICC) Dr Xu received his Ph.D. in Physiology from the Johns Hopkins University School of Medicine. Prior to joining JHICC, he served as vice president of research and development, and general manager of China operations at AVIVA Biosciences Corporation overseeing new product/service development programs in automated eletrophysiology, cardiac safety screening, and rare cell diagnosis. Prior to that, Dr. Xu was a senior scientist at Aurora Biosciences Corporation, leading assay development projects for major pharmaceutical partners.

Litao Zhang, Executive Director of Lead Evaluation and Mechanistic Biochemistry, Applied Biotechnology, BRISTOL-MYERS SQUIBB LITAO ZHANG is Executive Director of Lead Evaluation and Mechanistic Biochemistry, Applied Biotechnology, Bristol-Myers Squibb, Princeton, New Jersey, USA. She plays a leadership role of drug screening from hit identification to lead optimization and has accumulated more than 10 years of pharmaceutical industry experience with major pharmaceutical companies such as DuPont, Aventis and Bristol-Myers Squibb. Dr. Zhang is author of several publications and patents. She received her Ph.D. in Biochemistry from Washington University School of Medicine, Saint Louis, Missouri, USA.

Dr. Wei Zheng, Group Leader, NIH CHEMICAL GENOMICS CENTER Dr. Wei Zheng is a group leader at NIH Chemical Genomics Center working on lead discovery and optimization for research probes and drug development for rare diseases. Prior to NIH, He had worked for 12 years in pharmaceutical companies 12 years including Merck and Amgen. He has extensive experience in assay development, high throughput screening and lead optimization. Dr. Zheng received a Ph.D. degree in Biochemical Pharmacology at the State University of New York at Buffalo. He is the Editor-in-Chief of Current Chemical Genetics, a new open access journal focusing on the technologies and research related to the interface of chemical and biology.

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Drug Discovery: Easing the Chemistry Bottleneck June 8-9, 2009 sponsors >>>>>>>>>>>>>>>>>>>>>

Opal Events would like to thank its sponsors for their considerate support of Drug Discovery: Easing the Chemistry Bottleneck

Executive Sponsor ■ PANOMICS, recently acquired by Affymetrix, is a life science company that offers a platform of reagents and products that enable the multiplex measurement of molecular events, such as intracellular pathway analysis, cell signaling and gene expression profiling, in a quantitative and scalable manner. Panomics has grown rapidly on the value of its proprietary branched DNA technology for gene expression analysis in cell-based assays, as well as our signal transduction and transcription factor assays.

Panel Sponsor ■ CORNING LIFE SCIENCES is a leading developer, manufacturer and global supplier of scientific laboratory products. For more than 100 years, Corning has been the trusted partner of researchers seeking new approaches to increase efficiencies, reduce costs and compress timelines in the drug discovery process.Using our unique expertise in the combined fields of optics, materials science, surfaces, and biology, we provide a full range of innovative solutions that improve productivity and enable breakthrough discoveries. www.corning.com/lifesciences/

Exhibitor Sponsors ■ APREDICA provides discovery and early preclinical contract research services for the evaluation ■ CHEMDIV, INC. (CHEMDIV) is a global discovery and development and optimization of ADME-Tox and organization headquartered in San Pharmacokinetic properties of drug Diego, CA, USA with subsidiaries in candidates. Apredica maximizes the Russia, business and logistics speed and efficiency of drug- operations around the world. CHEMDIV discovery programs by providing fast turnaround and scientist-to-scientist is a provider of external integrated communications. Apredica's scientists have more than 10 years' drug- discovery and development solutions to pharma and biotech partners. discovery experience, and 80% have Ph.D.s, making Apredica an ideal Integrated Discovery outSourceÔ platform offered by CHEMDIV covers the partner for small and mid-sized drug-discovery companies, academic and complete range of disciplines needed to bring a project in CNS, oncology, government groups. inflammation, metabolic and infectious disease area from identification of a biological target (i.e. protein expression, assay development etc.); to ■ AsisCHEM is a global contract research organization that clinical drug candidates (ADME/PK, toxicity studies, efficacy models etc.); to provides custom synthesis and drug development candidate ( Phase I to Phase IV). Visit www.chemdiv.com medicinal chemistry services at for more information. competitive FTE rates. The company specializes in research-intensive ■ Nearing 20 years of experience CYBIO develops, produces and sells collaborations that are led by Ph.D.- technology platforms for drug level scientific project managers in the U.S. and carried out by a highly discovery and is an undisputed world experienced group of 30 Ph.D.-level chemists in St. Petersburg, Russia. The leader in simultaneous pipetting. By company offers the highest level of chemistry expertise, superior customer offering scalable systems for focus, exhaustive project management, complete quality control, and automated labs, CyBio provides relentless risk management. individual modules that can be fully integrated into complete solutions. CyBio automation is ideal for any procedure where miniaturization and ■ BIOMICROLAB offers affordable robotic systems, quality reagent conservation are important and CyBio is currently at the forefront control systems, and productivity tools of nano-liter liquid handling. primarily used by life scientists for In those laboratories where reliability and speed are paramount to the benchtop sample and compound process, CyBio instruments enjoy heavy use and represent an excellent management. BioMicroLab's robotic return on investment. Whether the needs are simultaneous liquid handling, instruments are complete systems for: precise imaging, or a walk-away answer for your specific application, CyBio (1) volume inventory management (2) sorting and weighing of vials and test is able to provide elegant and durable instruments and integrations for all tubes, and (3) 2D bar code decoding. BioMicroLab's robotic platforms are areas of HTS, genomics and proteomics. compatible with SBS standards to allow integration with HTS oriented laboratory systems.

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Drug Discovery: Easing the Chemistry Bottleneck notes >>>>>>>>>>>>>>>>>>>>>